(Carboxyacylamino)phenylalkenamides and esters thereof as SRS-A antagonists
AssigneePfizer Inc.
InventorSaul B. Kadin
Life of this patent
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Abstract
Certain new propenamides and 2-butenamides having a (carboxyalkanamido)phenyl or a (carboxyalkenamido)phenyl group at the 3-position, and certain esters thereof, and their use for antagonizing the spasmogenic activity of slow-reacting substance of anaphylaxis (SRS-A) in a human subject. In particular, the compounds of the invention are useful for preventing and treating certain obstructive airways diseases, notably allergic bronchial asthma, allergic rhinitis and certain skin disorders, in human subjects.
Claims27
An alkenamide compound of the formula ##STR27## and the pharmaceutically-acceptable salts thereof;
- wherein R.sup.1 is selected from the group consisting of hydrogen, alkyl having 1 to 4 carbons, and -CH.sub.2 -CH.sub.2 -NR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are each alkyl having 1 to 3 carbons;
- R.sup.2 is selected from the group consisting of alkyl having 8 to 15 carbons and cycloalkyl having from 6 to 12 carbons;
- R.sup.5 and R.sup.6 are selected from the group consisting of hydrogen and methyl;
- and X is selected from the group consisting of cis-vinylene, ethylene and ##STR28## wherein R.sup.7 and R.sup.8 are each selected from the group consisting of hydrogen and methyl.
The method of antagonizing the effect of slow-reacting substance of anaphylaxis in a human subject, which comprises administering thereto a slow-reacting substance of anaphylaxis antagonizing amount of an alkenamide compound of the formula ##STR30## or a pharmaceutically-acceptable salt thereof;
- wherein R.sup.1 is selected from the group consisting of hydrogen, alkyl having 1 to 4 carbons, and --CH.sub.2 --CH.sub.2 --NR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are each alkyl having 1 to 3 carbons;
- R.sup.2 is selected from the group consisting of alkyl having 8 to 15 carbons and cycloalkyl having from 6 to 12 carbons;
- R.sup.5 and R.sup.6 are selected from the group consisting of hydrogen and methyl;
- and X is selected from the group consisting of cis-vinylene, ethylene and ##STR31## wherein R.sup.7 and R.sup.8 are each selected from the group consisting of hydrogen and methyl.
A pharmaceutical composition, which comprises a pharmaceutically-acceptable carrier and an alkenamide compound of the formula ##STR32## or a pharmaceutically-acceptable salt thereof;
- wherein R.sup.1 is selected from the group consisting of hydrogen, alkyl having 1 to 4 carbons, and --CH.sub.2 --CH.sub.2 --NR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are each alkyl having 1 to 3 carbons;
- R.sup.2 is selected from the group consisting of alkyl having 8 to 15 carbons and cycloalkyl having from 6 to 12 carbons;
- R.sup.5 and R.sup.6 are selected from the group consisting of hydrogen and methyl;
- and X is selected from the group consisting of cis-vinylene, ethylene and ##STR33## wherein R.sup.7 and R.sup.8 are each selected from the group consisting of hydrogen and methyl;
- and wherein the ratio of the pharmaceutically-acceptable carrier to the alkenamide compound is in the range from 1:6 to 6:1 by weight.
Dependencies are inferred from the claim text.